| Summary: | Abstract
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The buccal mucosal route offers several advantages
but the delivery of certain drugs can be limited
by low membrane permeability. This study
investigated the buccal permeability properties
of didanosine (ddI) and assessed the potential of
Aloe vera gel (AVgel) as a novel buccal permeation
enhancer. Permeation studies were performed
using Franz diffusion cells, and the drug was
quantified by UV spectroscopy. Histomorphological
evaluations were undertaken using light and
transmission electron microscopy. The permeability
of ddI was concentration-dependent, and
it did not have any adverse effects on the buccal
mucosae. A linear relationship (R2 = 0.9557) between
the concentrations and flux indicated passive
diffusion as the mechanism of drug transport.
AVgel at concentrations of 0.25 to 2%w/v enhanced
ddI permeability with enhancement ratios
from 5.09 (0.25%w/v) to 11.78 (2%w/v) but
decreased permeability at 4 and 6%w/v. Ultrastructural
analysis of the buccal mucosae treated
with phosphate buffer saline pH 7.4 (PBS), ddI/
PBS, and ddI/PBS/AVgel 0.5%w/v showed cells
with normal plasmalemma, well-developed cristae,
and nuclei with regular nuclear envelopes.
However, cells from 1, 2, and 6%w/v AVgel-treated
mucosae showed irregular nuclear outlines, increased
intercellular spacing, and plasmalemma
crenulations. This study demonstrates the potential
of AVgel as a buccal permeation enhancer for
ddI to improve anti-HIV and AIDS therapy.
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